JP2003183123A - Skin care preparation for beautifully whitening skin and preparation method for the same - Google Patents

Abstract

<P>PROBLEM TO BE SOLVED: To provide a skin care preparation for external use for sufficiently beautifully whitening the skin which contains an extracted product of Glycyrrhiza urarelensis Fischer (or Glycyrrhiza glabra L var. glandulifera REG. et HERD) obtained by extracting the plant with an aqueous solvent. <P>SOLUTION: The skin care preparation for external use for beautifully whitening the skin is formulated with, as the effective ingredient, a transparent extracted product obtained by extracting Glycyrrhiza uralensis Fischer (or Glycyrrhiza glabra L var. glandulifera REG. et HERD) or a crude drug mixture of the Glycyrrhiza uralensis Fischer (or Glycyrrhiza glabra L var. glandulifera REG. et HERD) with Bupleurum chinense DC by using an aqueous solvent by heating at 100°C or higher, then subjecting the separated extracted product to filtration through activated carbon for removing the suspended matters therein. The above essential ingredients are selectively remained in the preparation, so that the effect to beautifully whiten the skin can be exhibited sufficiently. <P>COPYRIGHT: (C)2003,JPO

Description

Detailed Description of the Invention

[0001]

TECHNICAL FIELD The present invention relates to a whitening skin external preparation such as a cosmetic which prevents pigmentation of the skin or makes the deposited pigment pale.

[0002]

2. Description of the Related Art Melanin pigment, which is usually present in the epidermis of the skin, is produced by pigment cells and metabolized to the skin (2
It is naturally excreted every 8 days, but if the metabolic function does not work sufficiently after exposure to a large amount of ultraviolet rays, melanin pigment is deposited in the epidermis and dermis, and abnormal pigments appear on the skin such as spots and freckles. Deposition occurs.

Conventional whitening cosmetics include licorice extract, placenta extract, ascorbic acid and the like. It is known that these active ingredients have an effect of activating metabolic function when taken into the skin and preventing deposition of melanin pigment.

In addition, it is possible to blend an extract from licorice into cosmetics to prevent spots, for example, Japanese Patent Laid-Open No. 61-1222.
No. 09 and Japanese Patent Laid-Open No. 63-23809.

In the techniques disclosed in these documents, licorice extract prescribed in the local law was extracted from licorice (liquorice) using ethanol as an extraction solvent.

By the way, the licorice extract prescribed by the local law is
To 1 kg of finely sliced licorice, add 5 liters of normal water or purified water and soak it in the cold for 2 days. Strain it, add 3 liters of normal water or purified water, soak it for 12 hours, then strain it and combine the filtrates. After evaporating to 3 liters and cooling, 1 liter of ethanol was added, and the mixture was left for 2 days in a cold place and then filtered, and the filtrate was evaporated to obtain a soft extract.

[0007]

However, in such a method for producing local extract, since the filtering operation is performed by centrifugation or by wiping with a cloth, fine particles and substances having a small specific gravity are insoluble in water. Remains in the extract as a suspended substance. In addition, such a conventional licorice extract has an unstable action of suppressing the deposition of melanin pigment, and the effect is largely different among individuals, and it is not easy to exert a definite whitening effect.

The inventor of the present application has studied the above-mentioned licorice extract and its action. As a result, the local licorice extract contains many extracts because ethanol is used as an extraction solvent. Thought that many components are not always necessary, and rather many components cause complicated reactions, and the whitening effect originally to be obtained is not sufficiently exerted.

Therefore, the object of the present invention is to solve the above-mentioned problems, and in an external whitening agent for whitening containing an aqueous solvent extract of licorice, the ingredients necessary for whitening are selectively contained,
Efficient and sufficient whitening action, and efficient production of such a whitening external skin preparation.

[0010]

In order to solve the above problems, in the present invention, a transparent extract obtained by separating a suspended substance from an aqueous solvent extract of licorice, which is a crude drug, is contained as an active ingredient. It was used as an external preparation for whitening skin.

Although the mechanism of action of the whitening skin external preparation comprising the above components is not sufficiently clear, the concentration of glycyrrhizin and liquiritin after filtration with activated carbon is about 1/1000 that of licorice extract (Japanese Pharmacopoeia). However, it is considered that the filtrate does not contain other competing components or inactive components in view of efficiently exhibiting the whitening effect. A transparent liquid such as a filtrate from which suspended solids have been removed by at least activated carbon filtration is usually insoluble in the water contained by the licorice extract (Japanese Pharmacopoeia) being filtered by centrifugation or through a cloth. It does not contain fine particles or suspended substances consisting of low specific gravity substances,
These are considered to be competing or inactive components.

That is, in the invention relating to the whitening skin external preparation described above, among the components extracted with the aqueous solvent extract of licorice, a trace amount of a non-water-soluble solid which is present as a suspended substance in the extract. Since even the components are completely separated and removed, it is a whitening skin external preparation containing only a water-soluble component free from impurities that would limit the action of the present invention.

Therefore, an external preparation for skin comprising a whitening active ingredient selected in a smaller amount than in the past can sufficiently exert the whitening effect which should be obtained, as will be apparent from the experimental results described later.

The whitening effect is exhibited particularly reliably in the above-mentioned whitening skin external preparation when the separation is separation by filtration with activated carbon.

In order to solve the above-mentioned problems, a whitening skin external preparation containing as an active ingredient a transparent extract obtained by separating a suspended substance from an aqueous solvent extract of licorice and saiko, which are crude drugs. It was.

In the invention relating to the above-mentioned whitening skin external preparation, among the components extracted with the aqueous solvent extract of licorice and saiko, a trace amount of a water-insoluble substance that is present as a suspended substance in the extract is used. The solid components are completely separated and removed to give a skin external preparation containing only impurities-free water-soluble components as whitening active ingredients.

Therefore, as a whitening active ingredient, the whitening skin external preparation of the present invention comprising less components than conventional ones is
As is clear from the experimental results described below, the whitening effect of licorice and saiko, which should be obtained originally, is fully exerted.

As described above, the reliable whitening action is more reliably exhibited in the above-mentioned whitening skin external preparation when the separation is separation by filtration with activated carbon.

In addition, as a method for producing the above-mentioned whitening skin external preparation, licorice which is a crude drug or a mixed crude drug in which licorice and Saiko are mixed is extracted with an aqueous solvent heated to 100 ° C. or higher,
A method for producing a whitening skin external preparation may be employed in which a transparent extract obtained by filtering a separated extract with activated carbon is added as an active ingredient.

In the whitening skin external preparation having the above-mentioned constitution, licorice is extracted with warm water or hot water, impurities are removed by using activated carbon as a filtering material, and then a whitening cosmetic is prepared using this extract. Further, a whitening cosmetic composition can be prepared by treating a mixture of licorice and Saiko with the above method.

[0021]

BEST MODE FOR CARRYING OUT THE INVENTION Licorice used in the present invention is licorice which is a medicinal plant of the legume family produced in Spain, Siberia, China and the like, and has a scientific name of Glycyrrhiza urarelensis Fische.
r) or Glycyrrhiza glabra
L.var.glandulifera REG.et HERD) or roots or rhizomes of these closely related species (also known as grape vines or strons), either unpeeled or dry, excluding cork skin, powdered It is used as a component of the external preparation for the skin, either in the form of a strip or extracted with an aqueous solvent.

Saiko, which is used as another component of the external preparation for skin in the present invention, is Mishima Psycho of the Umbelliferae family, scientific name:
Bupleum falcatum
L.) or a root of a closely related species thereof, which is a dried herbal medicine, which can be used in a pulverized powder form, an extract extracted with an aqueous solvent, or the like.

The above crude drug may be dried for the purpose of enhancing the preservability, or may be powdered by crushing or grinding.

The aqueous solvent for extracting the active ingredient is water (which may be neutral, weak acid or weak alkaline) or an aqueous extraction solvent containing water as a main component,
An aqueous solution containing alcohol can also be adopted.

The aqueous solvent is preferably used in the extraction operation in the state of hot water or hot water in an efficient manner, and particularly at 100 ° C.
As described above, it has been found that the components effective for whitening are efficiently extracted by performing the extraction operation preferably at 100 to 130 ° C.

The obtained extract is filtered using a porous material such as activated carbon as a filter material, or is subjected to solid-liquid separation by utilizing the difference in specific gravity between solid and liquid and the difference in sedimentation rate due to gravity or centrifugal force. The suspended substance may be removed.

The activated carbon used in the present invention is not particularly limited in its material, but charcoal, bamboo or coconut shell as a raw material has a good adsorption efficiency for a suspended substance composed of fine particles. Is preferable.

As described above, the filtration operation is carried out by passing the extract through a container such as a column packed with activated carbon particles, or by adding activated carbon powder (if necessary, a filter aid such as talc) to the extract. In addition, a method of filtering the agitated mixture with a filter that captures the powder particles of the activated carbon such as a filter paper or a filter cloth can also be adopted, and other means such as centrifugation or separation due to a difference in sedimentation speed is adopted. You can also

In order to mix the liquid filtrate obtained by solid / liquid separation as an active ingredient, the extract is used as a base for a skin external preparation having a suitable hydrophilic / lipophilic property and good skin adhesion. It is preferable to mix or mix the extract with cream, ointment, emulsion and the like.

The form of the external preparation for skin is not particularly limited, but it is water-soluble, emulsion (skin milk), cream,
Formulation forms such as ointments and powders that are easy to apply are preferred.

[0031]

[Examples and Comparative Examples] [Examples 1 to 3 and Comparative Example]
1,500 grams of licorice and 10 to 15 liters of purified water were placed in a stainless steel container, heated to 100 ° C. and decocted for 30 minutes to extract, and 1500 g of activated carbon (Wako Pure Chemical Industries:
Activated carbon powder) is added and well stirred, and further 3000 g
Talc (manufactured by Maruishi Pharmaceutical Co., Ltd.) was added and stirred, and then filtered through filter paper, and the obtained filtrate was heated (100 ° C. or lower) and concentrated to a tar-like form.

Hydrophilic ointment (manufactured by Hishiyama Pharmaceutical Co., Ltd.) was added to the obtained concentrate to prepare a 15% cream.

In Example 2, a cream was prepared under the same conditions as in Example 1 except that the extraction temperature was 120 ° C.

In Example 3, 1500 grams of licorice and 1 of saiko
A cream was prepared in the same manner as in Example 2, using 500 g of the extract material together.

As Comparative Example 1, a licorice extract (Japanese Pharmacopoeia) was added to a hydrophilic ointment (manufactured by Hishiyama Pharmaceutical Co., Ltd.) to give 15
% Cream was made.

As Comparative Example 2, a cream was prepared in the same manner as in Example 2 except that 1500 grams of Saiko was used as the extraction material instead of the licorice in Example 2.

For reference, the contents of glycyrrhizin and liquiritin of each concentrated solution or licorice extract are shown in Table 1 below.

[0038]

[Table 1]

As is clear from the results shown in Table 1, liquiritin is a standard substance for licorice quality labeling similar to glycyrrhizin, and in the case of Japanese licorice extract, glycyrrhizin is 4.5% (45 mg). / g) or more. Here, as is clear from the results shown in Table 1, the extract obtained by filtering licorice and its aqueous solution contains glycyrrhizin in an amount of 1/2000 or less as compared with the licorice extract of Comparative Example 1, and liquiritin 1
It is / 400 or less, and it can be seen that the extract is completely different from the conventional licorice extract.

Further, since the contents of glycyrrhizin and liquiritin are completely different between the examples and the comparative examples, it is presumed that the compositions have different characteristics. In addition, since the content ratios of glycyrrhizin and liquiritin are different between Example 1 and Example 2, it is estimated that the compositions have different characteristics.

The obtained Examples 1 to 3 and Comparative Examples 1 and 2 were obtained.
The above external cream for skin was applied daily to the panelists (adults) each having a stain on their face by the number of cases shown in Table 2, and a questionnaire survey was conducted on the effect of improving the color of the stain after one month of use. The results are scored according to the following evaluations and are also shown in Table 2. Very Efficient: The person and others also feel thin. Effective: Either the person or another person feels thin. Somewhat effective: I feel that either the person or another person may have become thin. Invalid: Neither the person nor the other person feels thin. Invalid: 0 points Moderately effective: 1 point Effective: 2 points Very effective: 3 points

[0042]

[Table 2]

Further, as is clear from the results of Table 2,
It was found that the efficacy was enhanced in the order of Comparative Example 1, Example 1, Example 2, and Example 3, and in Examples 1 to 3, the evaluation point was 0.92 or more, which was an effective whitening effect.

On the other hand, in Comparative Example 1, only half or less of the evaluation points of Example 1 having the lowest evaluation score were obtained. Further, it is considered that the density of Comparative Example 2 did not have a substantially effective whitening effect.

Next, the tyrosinase activity inhibition rates of Examples 2 and 3 and Comparative Example 2 were measured by the following absorbance method. <Tyrosinase activity inhibitory activity by absorbance method (calculation of inhibition rate)> Mushroom-derived tyrosinase manufactured by Funakoshi Co., Ltd. was used to examine the tyrosinase activity inhibitory activity using the following reagents AE. A. L-tyrosine solution (0.5 mg / ml) 0.1 ml B.I. 1/5 M phosphate buffer (pH 7.0) containing 7.8 mM ascorbic acid 0.025 ml C.I. 0.1% copper sulfate solution 0.025 ml D.I. Tyrosinase solution (37.5 mg / 100 ml) 0.02 ml E. 0.1 ml of diluted sample solution

The enzyme reaction was carried out by FALC using a multi-plate reader (multi-scan ascent) manufactured by Dainippon Pharmaceutical Co., Ltd.
The reaction was performed in a 96-well multiwell plate manufactured by ON and the absorbance was measured. That is, first A, B, C, D, E
Each solution was added and the absorbance (Ao) at 620 nm at 0 hours was measured. Then, the mixture was incubated at 37 ° C. for 1 hour, and the absorbance (At) at 620 nm was measured again. At the same time, prepare a solution to which 0.1 ml of purified water was added instead of solution E,
The same reaction was performed to measure the absorbance (Ab), and the tyrosinase activity inhibition rate was calculated according to the following formula. Inhibition rate (%) = [Ab− (At−Ao) / Ab] × 10
0

The concentrations and inhibition rates of Examples 2 and 3 and Comparative Example 2 were plotted on a graph, and the respective concentrations required for 50% inhibition were measured. Table 3 shows the concentrations required for Example 2, Example 3 and Comparative Example 2 to inhibit 50% tyrosinase activity.

[0048]

[Table 3]

As is clear from the results in Table 3, the concentration required for 50% tyrosinase activity inhibition in Example 3 in which licorice and Saiko were used in combination was higher than that in Example 2, which was an extract containing only licorice. However, adding sycamore to licorice does not enhance the tyrosinase activity inhibitory effect.

However, as is clear from the results shown in Table 2 above, the whitening effect of Example 3 is superior to that of Example 2, so that the whitening effect is due only to the tyrosinase activity inhibiting effect. It can be inferred that other factors, for example, the water-soluble liquid component contained in Saiko enhances the whitening effect of licorice.

[0051]

The invention relating to the whitening skin external preparation of the present application is
As described above, since the transparent extract obtained by separating the suspended substance from the aqueous solvent extract of licorice, which is a crude drug, is contained as an active ingredient, the components necessary for whitening remain selectively. Therefore, there is an advantage that the whitening effect is exerted efficiently and efficiently, and the whitening effect is sufficiently and surely exhibited.

In addition, in the invention relating to the whitening skin external preparation of the present application, which uses licorice and licorice as an extraction material, the whitening effect is more reliably exhibited by the action of the active ingredient of licorice in addition to the above advantages.

Furthermore, in the invention relating to the method for producing a whitening skin external preparation of the present application, the extraction operation is performed at a predetermined temperature, so that the active ingredient is surely contained in a sufficient amount to ensure the whitening effect. It is possible to efficiently produce an external preparation for whitening skin.

Claims (5)

[Claims] 1. A whitening skin external preparation containing as an active ingredient a transparent extract obtained by separating a suspended substance from an aqueous solvent extract of licorice, which is a crude drug. 2. The whitening skin external preparation according to claim 1, wherein the separation is separation by filtration with activated carbon. 3. A whitening skin external preparation containing, as an active ingredient, a transparent extract obtained by separating a suspended substance from an aqueous solvent extract of licorice and Saiko, which are crude drugs. 4. The whitening skin external preparation according to claim 3, wherein the separation is separation by filtration with activated carbon. 5. A licorice, which is a crude drug, or a mixed crude drug, which is a mixture of licorice and Saiko, is extracted with an aqueous solvent heated to 100 ° C. or higher, and a transparent extract obtained by filtering this is added as an active ingredient. A method for producing an external preparation for whitening skin.